A century-old one-pot multicomponent Biginelli reaction products still finds a niche in drug discoveries: Synthesis, mechanistic studies and diverse biological activities …

S Faizan, TF Roohi, RM Raju, Y Sivamani… - Journal of Molecular …, 2023 - Elsevier
One of the largest classes of organic molecules are dihydropyrimidines and its derivatives.
They are widely used in a variety of pharmacological and industrial applications. Their …

Novel 4-(2-arylidenehydrazineyl) thienopyrimidine derivatives as anticancer EGFR inhibitors: Design, synthesis, biological evaluation, kinome selectivity and in silico …

HA Elsebaie, EA El-Bastawissy, KM Elberembally… - Bioorganic …, 2023 - Elsevier
The current study discovered fifteen new thieno [2, 3-d] pyrimidine derivatives with potential
anticancer action, including 5a-l, 6, and 7a-b. Results from the NCI screening revealed that …

[HTML][HTML] Advances in the discovery of DHPMs as Eg5 inhibitors for the management of breast cancer and glioblastoma: A review

D Nikam, A Jain - Results in Chemistry, 2023 - Elsevier
Breast cancer and gliobalstoma are the most aggressive types of diseases causing serious
health issues. Potent anticancer molecules are facing serious side effects which arouse the …

Synthesis, in vitro anticancer activity, and pharmacokinetic profiling of the new tetrahydropyrimidines: Part I

E Milović, JT Ristovski, S Stefanović… - Archiv der …, 2024 - Wiley Online Library
Different vanillin‐based aldehydes were used to synthesize novel tetrahydropyrimidines
(THPMs) via conventional Biginelli reaction. The THPMs were tested against human normal …

[HTML][HTML] Synthesis, evaluation of the cytotoxicity, apoptosis induction in AGS cell line and gene expression and molecular modeling studies of novel …

S Sepehri, Y Panahi, D Abbasi, M Jafari… - Arabian Journal of …, 2024 - Elsevier
Cancer is a complex disease that remains a leading cause of death worldwide owing to the
lack of effective and efficient drugs. Compounds known as tetrahydropyrmidine have shown …

Synthesis, crystal structure and molecular docking study of new monastrol analogues as inhibitors of epidermal growth factor receptor tyrosine kinase

SS Wazalwar, AR Banpurkar, F Perdih - Journal of Molecular Structure, 2023 - Elsevier
New dihydropyrimidone scaffolds were synthesized by Biginelli reaction aiming minor
structural modifications of anti-cancer drug monastrol. The benzaldehyde part was chosen …

Role of KSP inhibitors as anti-cancer therapeutics: an update

R Chamariya, V Suvarna - Anti-Cancer Agents in Medicinal …, 2022 - ingentaconnect.com
Regardless of the growing discovery of anticancer treatments targeting cancer-specific
pathways, cytotoxic therapy still maintained its abundant clinical significance because …

Chlorine containing tetrahydropyrimidines: Synthesis, characterization, anticancer activity and mechanism of action

E Milović, IZ Matić, N Petrović, I Pašić, T Stanojković… - Bioorganic …, 2024 - Elsevier
The aim of the presented research was to explore anticancer potential of eleven newly
synthesized tetrahydropyrimidine derivatives. The compounds were synthesized via Biginelli …

From beverage to anticancer agent: The repurposing of green coffee bean extract loaded in solid lipid nanoparticles

YA Moussa, MH Teaima, MM Elmazar, DA Attia… - Journal of Drug Delivery …, 2024 - Elsevier
Green coffee bean extract (GCBE) captivated the world with its various health benefits.
However, its topical use was limited by the hampered penetration of hydrophilic GCBE …

Synthesis, biological evaluation, docking and molecular dynamics studies of Biginelli-type tetrahydropyrimidine analogues: Antimicrobial, cytotoxicity and antioxidant …

S Sepehri, M Miran, F Mansouri, P Saeedkhani… - Journal of Molecular …, 2025 - Elsevier
Tetrahydropyrimidines have a fascinating scaffold that has garnered substantial attention
from pharmacists and medicinal chemists. They are heterocyclic compounds used in anti …